Synthesis and Structure—Activity Relationship of a New Series of COX-2 Selective Inhibitors:...
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2003 Imidazole derivatives Imidazole derivatives R 0190 Synthesis and Structure—Activity Relationship of a New Series of COX-2 Selec- tive Inhibitors: 1,5-Diarylimidazoles. — A wide variety of 1,5-diarylimidazoles such as (IV)-(VI) are prepared, involving as key reaction the cyclization of an imine with an isocyanide. In the cases where no electron-withdrawing group is present in the imine, the more reactive benzotriazolylmethyl isocyanide is more suitable than the tosylme- thyl isocyanide. The latter compound works well in the presence of the methylsulfonyl or sulfonamide moiety. The new compounds are evaluated both in vitro and in vivo for their cyclooxygenase-2 inhibiting activity, leading to compound (IV) as best candidate for clinical trials. — (ALMANSA*, C.; et al.; J. Med. Chem. 46 (2003) 16, 3463-3475; Res. Cent., Grupo Uriach, E-08184 Palau-Solita i Plegamans, Spain; Eng.) — Klein 45- 104
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Transcript of Synthesis and Structure—Activity Relationship of a New Series of COX-2 Selective Inhibitors:...
2003 Imidazole derivatives
Imidazole derivativesR 0190 Synthesis and Structure—Activity Relationship of a New Series of COX-2 Selec-
tive Inhibitors: 1,5-Diarylimidazoles. — A wide variety of 1,5-diarylimidazoles such as (IV)-(VI) are prepared, involving as key reaction the cyclization of an imine with an isocyanide. In the cases where no electron-withdrawing group is present in the imine, the more reactive benzotriazolylmethyl isocyanide is more suitable than the tosylme-thyl isocyanide. The latter compound works well in the presence of the methylsulfonyl or sulfonamide moiety. The new compounds are evaluated both in vitro and in vivo for their cyclooxygenase-2 inhibiting activity, leading to compound (IV) as best candidate for clinical trials. — (ALMANSA*, C.; et al.; J. Med. Chem. 46 (2003) 16, 3463-3475; Res. Cent., Grupo Uriach, E-08184 Palau-Solita i Plegamans, Spain; Eng.) — Klein
45- 104
